Slováková A, Hutt A J
Katedra chemickej teórie lieciv, Farmaceutická Fakulta Univerzity Komenského, Bratislava.
Ceska Slov Farm. 1999 May;48(3):107-12.
The present contribution to the problems of the stereochemistry of drugs is an attempt at stressing the importance of a stereochemical view of pharmacology and at informing about the advances of "chiral pharmacology" within the framework of the contemporary knowledge of selective effects of drugs. There are no simple solutions in the "racemates versus enantiomers" problems and each substance must be considered and tested individually, i.e. on the case-by-case principle. For many racemates available at present there exist relatively few items of knowledge concerning the pharmacological, toxicological and pharmacokinetic properties of their individual enantiomers, or concerning the influence of age, health condition, sex and genetic factors on biological availability and response of the organism to the drug. Additional testing of the enantiomers of the racemates used in practice can lead to the discovery of new indications of the original drug, improve its clinical use and result in increasing its safety and efficacy. If it is so, in this case the "chiral meditations" in pharmacology are double worth the problems they pose.
本文对药物立体化学问题的探讨，旨在强调药理学中立体化学观点的重要性，并在当代药物选择性作用知识的框架内，介绍“手性药理学”的进展。在“外消旋体与对映体”问题上没有简单的解决方案，每种物质都必须单独考虑和测试，即根据具体情况原则。对于目前可用的许多外消旋体，关于其单个对映体的药理、毒理和药代动力学性质，或关于年龄、健康状况、性别和遗传因素对生物利用度以及机体对药物反应的影响，所知相对较少。对实际使用的外消旋体的对映体进行额外测试，可能会发现原药物的新适应症，改善其临床应用，并提高其安全性和有效性。如果是这样，那么在这种情况下，药理学中的“手性思考”所带来的问题就很值得了。
